The present invention relates to a series of new 1-[(2-benzhydryloxyethyl)-4-piperidyl]aliphatic acid derivatives which have excellent anti-histamine, anti-allergic and anti-asthma activities without exhibiting the side effects so common with compounds having this type of activity. The invention also provides methods and compositions using these compounds as well as processes for their preparation.
Certain 1-[(2-benzhydryloxyethyl)-4-piperidyl]acetic acid derivatives having an activity similar to that of the compounds of the present invention are disclosed in Japanese Patent Application Kokai No. Sho. 63-68564 (equivalent to European Patent Publication No. 259 227), but the activities of the compounds of the present invention are substantially better than those of the compounds of this prior art; the compounds of the present invention also have a potent inhibitory effect on the accumulation of eosinophile in the bronchoalveolar lavage fluid and do not have the side effects common to most anti-histamines, notably sedative effects (commonly drowsiness), dryness of the oral mucosa etc. They also have a low toxicity and are therefore expected to find widespread applications in the treatment and prophylaxis of histamine-related disorders. Particularly asthma and allergies.
In addition to the prior art referred to above, Japanese Patent Application Kokai No. Hei. 2-212472, which was published after the priority dates hereof, but before the filing date, discloses certain 1-[(2-benzhydryloxyethyl)-4-piperidyl]acetic acid derivatives which have an activity similar to that of the compounds of the present invention, but which are different in that the compounds of the present invention possess other aliphatic acid groups than the acetic acid group of the prior art compounds.